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詳細
Carboxylesterase 2 human gene is mapped to human chromosome 16q22.1.
Carboxylesterase belongs to the α/β hydrolase fold family and is involved in drug metabolism and activation. It is present in colon, liver, small intestine, heart, brain and testis. The hydrolase activity of small intestine is attributed to carboxylesterase 2 human. It has two glycosylation sites at 103 and 267 residues with molecular mass 60kDa.
アプリケーション
Carboxylesterase 2 human has been used:
- in the in vitro enzyme-based inhibitor screening assay
- in substrate selectivity assay with emission ratiometric two-photon probe (SE1)
- as a reference standard in the enzyme assay with various 4-nitrophenyl and 1-naphthyl based substrates
Carboxylesterase 2 may play a key role in biotransformation of a variety of ester containing drugs and prodrugs.
Delivers high catalytic activity, ideal for robust high-throughput screening assays including drug-drug interaction studies, and pharmacokinetic studies for evaluating pro-drugs and non-CYP pathways of elimination.
生物化学的／生理学的作用
Carboxylesterase 2 human identifies the site containing a large alcohol and small acyl group. It shows less transesterification activity due to presence of conformational interference in active site.
セリンエステラーゼファミリーのメンバーであり、エステルおよびアミド結合を加水分解します。カルボキシエステラーゼ2は、小胞体結合型加水分解酵素であり、エステル含有治療のための生体異物の解毒および活性化において重要な役割を果たします。また、カルボキシエステラーゼ2は、ヘロインやコカインなどの薬物の解毒にも関与します。本酵素は、脂質代謝において役割を担っていると考えられています。
単位の定義
One unit will produce 1 nanomole of 4-nitrophenol from 4-nitrophenyl acetate per minute at pH 7.4 at 37 deg C.
保管分類コード
10 - Combustible liquids
WGK
nwg
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
カルタヘナ法
カルタヘナ法
Jan Code
E0412-VAR:
E0412-1VL:
E0412-1VL-PW:
E0412-BULK:
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Human liver carboxylesterase. Purification and molecular properties.
W Junge et al.
Archives of biochemistry and biophysics, 165(2), 749-763 (1974-12-01)
T Satoh et al.
Annual review of pharmacology and toxicology, 38, 257-288 (1998-05-23)
Multiple carboxylesterases (EC 3.1.1.1) play an important role in the hydrolytic biotransformation of a vast number of structurally diverse drugs. These enzymes are major determinants of the pharmacokinetic behavior of most therapeutic agents containing ester or amide bonds. Carboxylesterase activity
Tetsuo Satoh et al.
Drug metabolism and disposition: the biological fate of chemicals, 30(5), 488-493 (2002-04-16)
This article reports on a symposium sponsored by the American Society for Pharmacology and Experimental Therapeutics and held at the April 2001 Experimental Biology meeting. Current developments in molecular-based studies into the structure and function of cholinesterases, carboxylesterases, and paraoxonases
Teruko Imai
Drug metabolism and pharmacokinetics, 21(3), 173-185 (2006-07-22)
Human carboxylesterase 1 (hCE-1, CES1A1, HU1) and carboxylesterase 2 (hCE-2, hiCE, HU3) are a serine esterase involved in both drug metabolism and activation. Although both hCE-1 and hCE-2 are present in several organs, the hydrolase activity of liver and small
Jianqin Zhang et al.
Chemosphere, 93(6), 1207-1215 (2013-08-01)
Carboxylesterases (CarEs) play key roles in metabolism of specific hormones and detoxification of dietary and environmental xenobiotics in insects. We sequenced and characterized CarE cDNAs putatively derived from two different genes named LmCesA1 and LmCesA2 from the migratory locust, Locusta
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